Publications by authors named "A Bakuridze"

41 Publications

FORMULATION THERMORESPONSIVE NANOCOMPOSITE HYDROGELWITH EMBEDDED PLGA NANOPARTICLES CONTAINING CYTOTOXIC AGENT.

Georgian Med News 2021 Mar(312):133-138

Tbilisi State Medical University, Faculty of Pharmacy, 1Department of Pharmaceutical Technology; Georgia.

The aim of the study was to develop and characterize the nanocomposite in-situ hydrogel as local drug delivery system of cytotoxic agent. In-situ hydrogel consisting of 15% thermosensitive (Poloxamer 407) and 1% mucoadhesive (sodium alginate) polymers was selected as the optimal formulation by the conducted studies. The influence of nanoparticle concentration on gelation time and temperature has been experimentally established. As a result, the optimum concentration of nanoparticles (5%) is selected, which does not alter the gel forming process. The resulting nanocomposite hydrogel was characterized through Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), rotational viscometer (LVDV-1T). FT-IR spectra confirmed the PLGA nanoparticles presence within the hydrogel matrix through the absorption peak located at 1750 cm-1. SEM images allowed observing the nanoparticles to be homogenously dispersed. The release pattern of the active substance from the nanocomposite hydrogel is following: at 72 h, 64% and 78% of the active substance were released into the phosphate buffer and cell culture area, respectively. Irritation test on hen's egg model revealed that formulated nanocomposite hydrogel did not show damage of vascular system.
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March 2021

ANTIHYPERTENSIVE AND CARDIOPROTECTIVE EFFECTS OF EPOXYEICOSATRIENOIC ACID ANALOGS AND SOLUBLE EPOXIDE HYDROLASE INHIBITORS (REVIEW).

Georgian Med News 2021 Mar(312):125-132

Tbilisi State Medical University, Departments of Pharmaceutical Technology and Medical Pharmacology, Georgia.

In the present article is considered antihypertensive and cardioprotective action of epoxieicosatrienoic acids (EETs) analogues and soluble epoxide hydrolase (sEH) inhibitors. Being epoxygenase products of arachidonic acid metabolism EETs provide a wide spectrum of biological activity in different organs implicated in the regulation of arterial pressure, including vascular endothelium (VE), heart and kidney. EETs are acting as autocrine or paracrine agents producing vasodilation, reduction in salt and fluid retention. EETs exert vasodilatory properties by activation of the smooth muscle large conductance Ca2+ -activated K+ channels in different vascular beds. In experimental and clinical studies EETs provide beneficial influence in hypertensive states alleviating vascular endothelium function associated with reduction of inflammation and increased Na+ excretion, prevented cardiovascular and renal complications accompanied arterial hypertension (AH). In animals studies using Dahl-salt-sensitive (Dss) hypertensive rats EETs analogues displayed renoprotective effect, reducing mRNA expression of tumor growth factor-"B" as well as concomitant oxidative stress and fibrotic changes in the heart and kidneys. In cultered endothelial cells also was demonstrated anti-inflammatory action of EETs when they significantly decreased TNF-α-induced high level of monocyte chemoattractant protein-1, which was reversed by EETs antagonist. sEH is another new target for therapeutic intervention in cardiovascular diseases. In several experimental models of AH sEH inhibitors (sEHI) significantly reduce AP which was associated with their anti-inflammatory and renoprotective action. sEHI showed cardiovascular effect related to CYP2J2overexpression during myocardial ischemia-reperfusion injury. It should be noted that EETs demonstrate binding ability to PPAR receptor "Y" stimulating it's transcription process in endothelial cells facilitating by sEHI. It is suggested that EETs and sEH are involved in the regulation of the cardiovascular function playing significant role in vascular homeostasis.
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March 2021

BIOPHARMACEUTICAL UNDERSTANDING OF FORMULATION PREPARATION VARIABILITY OF PLGA NANOPARTICLES LOADED WITH ERYSIMUM EXTRACT.

Georgian Med News 2021 Feb(311):173-177

Tbilisi State Medical University, Faculty of Pharmacy, 1Department of Pharmaceutical Technology; Faculty of Pharmacy, 2Direction of Pharmacognosy and pharmaceutical botany, Georgia.

The purpose of this study was to evaluate effect of process and formulation variables on the preparation of Erysimum extract loaded PLGA nanoparticles. The influence of the various biopharmaceutical factors such as type of organic solvent, type and concentration of surfactant, polymer concentration in the organic phase, ratio of organic phase and water phase were studied. Modified emulsification solvent evaporation method was used for preparation of nanoparticles. Based on the performed experiments optimal formulation of nanocomposite is suggested. Nanoparticle size, size distribution and entrapment efficiency were determined. Among five non-ionic surfactants polyvinyl alcohol provided more stable nanocomposite. Influence mechanisms of different surfactants on nanoparticle formation are provided. Water miscible organic solvent, acetone obtained 232 nm nanoparticles with improved size distribution. Entrapment efficiency was increased to 73% by reducing ratio of organic and water phases. Based on experiments nanoparticles with stable, reproducible properties are fabricated.
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February 2021

; INTRODUCTION OF AROMATIC PLANTS IN THE BATUMI BOTANICAL GARDEN AND THEIR RESEARCH FOR THE CONTENT OF BIOLOGICALLY ACTIVE COMPOUNDS.

Georgian Med News 2020 Jul-Aug(304-305):153-157

Batumi Botanical Garden; Tbilisi State Medical University; Batumi Shota Rustaveli State University, Institute of phytopathology and Biodiversity, Georgia.

The research objectives were to study the introduction process of different aromatic and spice plants in the Batumi Botanical Garden and the content of bioactive compounds in aromatic plants introduced and grown in the soil and climatic conditions of the garden.; Among the aromatic plants introduced to the BBG by the authors, the following species are having full vegetative and generative development in the open ground:Cuminum cyminum L.; Polianthes tuberosa L.; Iris pallida Lam.;Geranium macrorrhizum L., Piper suaveolens Ham., Piper piperita L., Thymus citriodorus Schreb., Satureja Montana L., Mentha piperita L., Origanum vulgare L., Mentha longifolia L., Hyssopus officinalis L.; Phyla scaberrima Moldenke, Ruta graveolens L.; Vegetative organs reach the full development, but without blooming:Curcuma longa L..; Zingiber officinale Roscoe.; Elettaria cardamomum Maton.; Coffea arabica L.; Coffea conephera L..; Vanilla planifolia Jacks.; Cassia acutifolia Delile.; For the purpose of studying the content of bioactive compounds in plants introduced to the soil and climatic conditions of the BBG with the help of green technologies, the following species were taken for analysis:Cassia acutifolia Delile. - seed, flower, leaf; Cuminum cyminum L. - seed; Coffea conefera L. andCoffea Arabica L., leaves and seeds; Vanilla planifolia Jacks. - leaves; Elletaria cardamomum Maton. -Cardamom leaves.With the help of gas chromatography - mass spectrometry GC-MS method, there were identified bioactive compounds of various classes. The content of essential oils is identified in all research objects.
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September 2020

FORMULATION OF BIODEGRADABLE POLYMERIC NANOPARTICLES CONTAINING CYTOTOXIC SUBSTANCE OF PLANT ORIGIN.

Georgian Med News 2020 Feb(299):137-142

Tbilisi State Medical University, 1Department of Pharmaceutical Technology, Georgia.

Formulation of novel drug delivery system is one of the approaches for improvement of pharmacological activity of drugs. This implies encapsulation of the API into the biocompatible polymeric material. Objective of the research was formulation of biodegradable amino acid based polyesteramide nanoparticles composing cytotoxic substance of plant origin. Research materials and methods: biodegradable polyesteramide (PEA), alkaloids from Vinca Minor, surfactants (Tween 80, polyvinyl pirolidone, polyvinyl alcohol, Poloxamer 188). NPs size (mean particle diameter) and size distribution (polydispersity index, PDI), and zeta-potential (ZP) were measured by dynamic light scattering (DLS) using a Zetasizer Nano ZS (Malvern Instruments, U.K.) at 25°C, UV spectrophotometer was used for %EE study. Amino acid based PEA particles were fabricated by the modified emulsification method. Based on the studies optimal composition and fabrication condition of PEA NPs was determined. The conditions of the NPs fabrication were as follows: the O/W ratio: 1:10; the solvent: DMSO; polymer concentration in the organic phase: 50.0 mg/mL; surfactants (PVA) concentration in aqueous phase 0.5%,the stirring rate: 1000 rpm. The influence of the various factors such as organic solvents, surfactants, as well as a polymer concentration in the organic phase,surfactant concentration in the aqueous phase,the organic/water phase ratio on the NPs fabrication was studied.The NPs were characterized by size (mean particle diameter & size distribution (polydispersity index, PDI), and zeta-potential (ZP). Increase concentration of the surfactant (polyvinyl alcohol) from 0.1% to 0.5% decrease average particle size from 568±63 to 169±1.66 respectively. EE% was obtained to be around 50%.
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February 2020